Browse Items · NEOMED Bibliography Database

Nuclear receptor-mediated repression of human cholesterol 7alpha-hydroxylase gene transcription by bile acids.

Hydrophobic bile acids strongly repressed transcription of the human cholesterol 7alpha-hydroxylase gene (CYP7A1) in the bile acid biosynthetic pathway in the liver. Farnesoid X receptor (FXR) repressed CYP7A1/Luc reporter activity in a transfection…

Tags: *Hydroxysteroid Dehydrogenases, *Membrane Glycoproteins, 2001, Animals, Bile Acids and Salts/*pharmacology, Caco-2 Cells, Carrier Proteins/genetics/physiology, Cell Line, Chen W, Chiang J Y, CHO Cells, Cholesterol 7-alpha-Hydroxylase/*genetics, Cricetinae, Cultured, Cytoplasmic and Nuclear/genetics/*physiology, Department of Integrative Medical Sciences, DNA-Binding Proteins/drug effects/genetics/physiology, DNA/metabolism, Embryo, Gene Expression/*drug effects, Genetic, Genetic/drug effects, Humans, Journal of lipid research, Kidney, Liver/metabolism, Luciferases/genetics, Mammalian, Messenger/analysis, NEOMED College of Medicine, Owsley E, Promoter Regions, Rats, Receptors, Recombinant Fusion Proteins/metabolism, Retinoic Acid/genetics/physiology, Retinoid X Receptors, Reverse Transcriptase Polymerase Chain Reaction, RNA, Stroup D, Taurocholic Acid/pharmacology, Transcription, Transcription Factors/drug effects/genetics/physiology, Transfection, Tumor Cells, Yang Y

Functional selectivity of NK1 receptor signaling: peptide agonists can preferentially produce receptor activation or desensitization.

A cascade of events follows binding of an agonist ligand to the tachykinin NK(1) receptor. These events include activation of multiple signal transduction pathways as well as cellular modulation of receptor function by the process of desensitization.…

Tags: 2006, Animals, CHO Cells, Cricetinae, Dose-Response Relationship, Drug, Humans, Neurokinin-1/agonists/drug effects/*physiology, Rana catesbeiana, Rats, Receptors, Signal Transduction/*physiology, Simmons Mark A, Substance P/metabolism/pharmacology, Tachykinins/metabolism/pharmacology, The Journal of pharmacology and experimental therapeutics

Neurokinin-1 receptor resensitization precedes receptor recycling.

Following agonist binding, neurokinin-1 receptors undergo rapid desensitization followed by internalization and recycling. Desensitization requires receptor phosphorylation but does not require internalization, whereas resensitization is thought to…

Tags: 2005, Adenosine Triphosphate/pharmacology, Animals, Bennett V J, Binding, Calcium/metabolism, CHO Cells, Competitive, Cricetinae, Guanylyl Imidodiphosphate/pharmacology, Neurokinin-1/*metabolism, Perrine S A, Phosphorylation, Rats, Receptors, Simmons M A, Substance P/metabolism, The Journal of pharmacology and experimental therapeutics

A novel mechanism of neurokinin-1 receptor resensitization.

Prolonged or repeated activation of many G protein-coupled receptors induces rapid desensitization followed by a period during which receptors are resensitized. In this study, concanavalin A (Con A) and monensin were used to investigate the…

Tags: 2002, Animals, Bennett V J, Cell Membrane/drug effects/metabolism, CHO Cells, Concanavalin A/pharmacology, Cricetinae, Monensin/pharmacology, Neurokinin-1/*agonists/*metabolism, Perrine S A, Phosphorylation/drug effects, Rats, Receptors, Simmons M A, The Journal of pharmacology and experimental therapeutics

Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor.

The NK(3) subtype of tachykinin receptor is a G protein-coupled receptor that is a potential therapeutic target for several neurological diseases, including schizophrenia. In this study, we have screened compound databases for novel NK(3) receptor…

Tachykinin peptide-induced activation and desensitization of neurokinin 1 receptors.

The actions of four tachykinins on inhibition and desensitization of the

Tags: 2003, Amino Acid Sequence, Animals, Bennett V J, CHO Cells, Cricetinae, Down-Regulation/*drug effects, Electrophysiology, Ligands, Neurokinin-1/*agonists/*metabolism, Peptides, Perrine S A, Potassium/metabolism, Protein Binding, Rana catesbeiana, Receptors, Simmons M A, Tachykinins/chemistry/*pharmacology

The role of the N-terminal and mid-region residues of substance P in regulating functional selectivity at the tachykinin NK1 receptor.

Previous studies have shown that tachykinin peptide ligands of the tachykinin NK1 receptor exhibit functional selectivity with respect to signal activation and desensitization. The differences are most dramatic between the naturally occurring…

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